Clin Psychopharmacol Neurosci.  2011 Apr;9(1):9-16.

Central Nervous System Drug Evaluation Using Positron Emission Tomography

• Sekine M
• Maeda J
• Shimada H
• Nogami T
• Arakawa R
• Takano H
• Higuchi M
• Ito H
• Okubo Y
• Suhara T

Abstract

In conventional pharmacological research in the field of mental disorders, pharmacological effect and dose have been estimated by ethological approach and in vitro data of affinity to the site of action. In addition, the frequency of administration has been estimated from drug kinetics in blood. However, there is a problem regarding an objective index of drug effects in the living body. Furthermore, the possibility that the concentration of drug in blood does not necessarily reflect the drug kinetics in target organs has been pointed out. Positron emission tomography (PET) techniques have made progress for more than 20 years, and made it possible to measure the distribution and kinetics of small molecule components in living brain. In this article, we focused on rational drug dosing using receptor occupancy and proof-of-concept of drugs in the drug development process using PET.

Keyword

Positron emission tomography; Occupancy; Dopamine D2 receptor; Serotonin transporter; Norepinephrine transporter; micro-PET

MeSH Terms

Brain
Central Nervous System
Drug Evaluation
Electrons
Kinetics
Mental Disorders
Norepinephrine Plasma Membrane Transport Proteins
Positron-Emission Tomography
Receptors, Dopamine D2
Serotonin Plasma Membrane Transport Proteins
Norepinephrine Plasma Membrane Transport Proteins
Receptors, Dopamine D2
Serotonin Plasma Membrane Transport Proteins